Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment

a technology of n-heterocyclic carbene and complexes, applied in the field of platinum (ii) complexes containing n-heterocyclic carbene ligand and pincer ligand, synthesis, and their applications in cancer treatment, can solve the problems of hampered the wider application of these dna binding agents and failure to combat metastatic cancer, and achieve excellent bio-probes.

Active Publication Date: 2020-03-03
VERSITECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, severe side effects and the induced drug resistance are commonly encountered and thus subsequently have hampered the wider applications of these DNA binding agents.
Yet, most of them fail in combating with metastatic cancer, which is a big problem found in cancer treatment.

Method used

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  • Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment
  • Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment
  • Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment

Examples

Experimental program
Comparison scheme
Effect test

example 6.1

and Characterization of the NHC Complexes

[0122]The following examples illustrate the synthesis and characterization of the platinum(II) complexes.

[0123][Pt(BPI)(NHC)](OTf) with different alkyl chains and aromatic groups on the NHC ligands were prepared by refluxing [Pt(BPI)Cl][25] with corresponding imidazolium salt in the presence of base (FIG. 1; See Supporting Information for experimental details and characterization data). The structure of 1a was further examined by X-ray crystallography (FIG. 2 and Table 1) and the NHC ligand was found to be perpendicular to the plane of BPI ligand with bond angle (C19-Pt1-N5) of 90.6°.

[0124]

TABLE 1Crystal data and structure refinement data for 1a.Identification code1aEmpirical formulaC23H20N7Pt · CF3O3S*Formula weight738.62Temperature / K100Crystal systemmonoclinicSpace groupC2 / ca / Å24.5594 (9)b / Å14.9575 (6)c / Å15.7468 (6)α / °90.00β / °119.678 (1)°γ / °90.00Volume / Å35025.7 (3)Z8ρcalc g / cm31.515μ / mm−111.80F(000)2864.0Crystal size / mm30.06 × 0.02 × 0.02Ra...

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Abstract

Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer / tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

Description

1. INTRODUCTION[0001]Described herein are platinum (II) complexes containing N-heterocyclic carbene ligand, a method of synthesis of the platinum (II) complexes containing N-heterocyclic carbene ligand, methods of treating and preventing cancer or tumor using the platinum (II) complexes containing N-heterocyclic carbene ligand. The platinum (II) complexes has a dual action including cytotoxic to tumor growth and anti-angiogenesis. Also provided is a method of detecting the platinum(II) complexes containing N-heterocyclic carbene ligand by fluorescence microscopy. Also described are therapeutic and prophylactic compositions containing a purified platinum(II) complexes containing N-heterocyclic carbene ligand. In certain embodiments, the methods of treating and preventing cancer or tumor are in combination with other cancer or tumor treatment. In certain embodiments, the cancer or tumor treatment is chemotherapy, radiation therapy, gene therapy, surgery or a combination thereof.2. BAC...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): C07F15/00A61P35/00G01N33/574G01N21/64
CPCA61P35/00G01N21/6486G01N21/6458G01N33/57415C07F15/0086C07F15/0093
Inventor CHE, CHI MINGFUNG, SIN KICHEN, TIAN FENG
Owner VERSITECH LTD
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